Ezatiostat
Based on 8 publication(s) in Google Scholar
Ezatiostat (TER199 free base; TLK199) is a tripeptide analog of glutathione and is a selective and orally active glutathione S-transferase P1-1 (GSTP1) inhibitor. Ezatiostat leads to JNK activation by inhibiting GSTP1. Ezatiostat stimulates both lymphocyte production and bone marrow progenitor proliferation. Ezatiostat has the potential for myelodysplastic syndrome (MDS) treatment.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté: 99.71%
- CAS No.: 168682-53-9
- Formule: C27H35N3O6S
- Masse moléculaire:529.65
-
Stockage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Activité biologique
-
Chemical Information
-
Solvant et solubilité
- Pureté et documentation
- Références
-
Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Ezatiostat
More- Cell Res. 2018 Dec;28(12):1171-1185. [Abstract]
- Adv Sci (Weinh). 2023 Mar;10(7):e2205262. [Abstract]
- Redox Biol. 2024 Aug 20:76:103323. [Abstract]
- Redox Biol. 2023 May:61:102635. [Abstract]
- Phytomedicine. 2024 Aug 31:134:155989. [Abstract]
- Free Radic Biol Med. 2024 Jun 19:S0891-5849(24)00531-8. [Abstract]
- Arch Biochem Biophys. 2024 Jul:757:110043. [Abstract]
- Cancer Biomark. 2025 Oct;42(10):18758592251390145. [Abstract]
Customer Validation & Images
-
Bio/Physico-chemical Assay
-
WB
-
Cell Proliferation/Viability Assay
-
In Vivo Efficacy Study
-
Cell Proliferation/Viability Assay
Activité biologique
Glutathione S-transferase P1-1 (GSTP1)[1]
Ezatiostat causes dissociation of the enzyme from the jun-N-terminal kinase/c-Jun (JNK/JUN) complex, leading to JNK activation by phosphorylation. The therapeutic action of ezatiostat appears to include both proliferation of normal myeloid progenitors as well as apoptosis of the malignant clone[1].
Selection of a resistant clone of an HL60 tumor cell line through chronic exposure to Ezatiostat (TLK199) results in cells with elevated activities of c-Jun NH2 terminal kinase (JNK1) and ERK1/ERK2, and allowes the cells to proliferate under stress conditions that induced high levels of apoptosis in the wild type cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
-
CAS No. 168682-53-9
-
Appearance Solid
-
Masse moléculaire 529.65
-
Formule C27H35N3O6S
-
Color White to off-white
-
Synonyms
TER199free base; TLK199
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (8)
-
Journal Impact Factor
-
Most Recent
-
Cell Res
2018 Dec;28(12):1171-1185. PMID: 30287942 -
Adv Sci (Weinh)
Targeting GSTP1 as Therapeutic Strategy against Lung Adenocarcinoma Stemness and Resistance to Tyrosine Kinase Inhibitors. [Abstract]2023 Mar;10(7):e2205262. PMID: 36709476
Ezatiostat purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Mar;10(7):e2205262. [Abstract]
In vitro effects of treatment with the GSTP1 inhibitor Ezatiostat (12.5 μM) on crizotinib sensitivity in LUAD-OG1 evaluated by Cell titer-Glo cell viability assay.
Ezatiostat purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Mar;10(7):e2205262. [Abstract]
Schematic diagram of the treatment regimen with 1% Tween 80/saline (Group 1), crizotinib (10 mg/kg; Group2), ezatiostat (25 mg/kg; Group 3), or the combination of ezatiostat with crizotinib (Group 4) in NOD-SCID mice. n = 4 mice per group. Representative image of LUAD-OG1 xenografts from the four groups at the endpoint are shown.
Ezatiostat purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Mar;10(7):e2205262. [Abstract]
Ex vivo effects of GSTP1 inhibitor Ezatiostat (12.5 and 25 μM) treatment on crizotinib sensitivity in crizotinib-resistant LUAD-OG1 evaluated by Cell titer-Glo cell viability assay.
Ezatiostat purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Mar;10(7):e2205262. [Abstract]
Schematic diagram of oral gavage of the treatment regimen with 1% Tween 80/saline (Group 1), crizotinib (25 mg kg−1; Group2), ezatiostat (25 mg/kg; Group 3), or the combination of ezatiostat with crizotinib (Group 4) in SCID mice.
-
Redox Biol
Tryptanthrin targets GSTP1 to induce senescence and increases the susceptibility to apoptosis by senolytics in liver cancer cells. [Abstract]2024 Aug 20:76:103323. PMID: 39180983
Ezatiostat purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Aug 20:76:103323. [Abstract]
Huh7 cells were treated with 0, 5, 10, and 20 μM Ezatiostat (TLK199) for 72 h, followed by FACS analysis to assess ROS production.
Ezatiostat purchased from MedChemExpress. Usage Cited in: Redox Biol. 2024 Aug 20:76:103323. [Abstract]
Protein expression levels of Lamin B1, p21, γ-H2AX and H2AX were detected by western blot upon treatment of Ezatiostat (TLK199, 0-20 μM, 72 h), with β-actin as a loading control.
-
Redox Biol
GSTP1-mediated S-glutathionylation of Pik3r1 is a redox hub that inhibits osteoclastogenesis through regulating autophagic flux. [Abstract]2023 May:61:102635. PMID: 36870110 -
Phytomedicine
Galangin alleviated Doxorubicin-induced cardiotoxicity by inhibiting ferroptosis through GSTP1/JNK pathway. [Abstract]2024 Aug 31:134:155989. PMID: 39217656 -
Free Radic Biol Med
Mifepristone protects acetaminophen induced liver injury through NRF2/GSH/GST mediated ferroptosis suppression. [Abstract]2024 Jun 19:S0891-5849(24)00531-8. PMID: 38906233 -
Arch Biochem Biophys
Subcellular distribution and Nrf2/Keap1-interacting properties of Glutathione S-transferase P in hepatocellular carcinoma. [Abstract]2024 Jul:757:110043. PMID: 38789086 -
Cancer Biomark
TUBB3 (βIII-tubulin) drives gastric cancer progression and poor prognosis by regulating cell cycle and invadopodia formation. [Abstract]2025 Oct;42(10):18758592251390145. PMID: 41129675
Solvant et solubilité
DMSO : 100 mg/mL (188.80 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Ethanol : ≥ 100 mg/mL (188.80 mM)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.75 mg/mL (5.19 mM); Clear solution
This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.75 mg/mL (5.19 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.75 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation
-
Fiche technique (275 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Instruction de manipulation (2659 KB)
Références
[1]. Galili N, et al. Prediction of response to therapy with ezatiostat in lower risk myelodysplastic syndrome. J Hematol Oncol. 2012 May 6;5:20 [Content Brief]
[2]. Ruscoe JE, et al. Pharmacologic or genetic manipulation of glutathione S-transferase P1-1 (GSTpi) influences cell proliferation pathways. J Pharmacol Exp Ther. 2001 Jul;298(1):339-45. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / Ethanol | 1 mM | 1.8880 mL | 9.4402 mL | 18.8804 mL | 47.2010 mL |
| 5 mM | 0.3776 mL | 1.8880 mL | 3.7761 mL | 9.4402 mL | |
| 10 mM | 0.1888 mL | 0.9440 mL | 1.8880 mL | 4.7201 mL | |
| 15 mM | 0.1259 mL | 0.6293 mL | 1.2587 mL | 3.1467 mL | |
| 20 mM | 0.0944 mL | 0.4720 mL | 0.9440 mL | 2.3600 mL | |
| 25 mM | 0.0755 mL | 0.3776 mL | 0.7552 mL | 1.8880 mL | |
| 30 mM | 0.0629 mL | 0.3147 mL | 0.6293 mL | 1.5734 mL | |
| 40 mM | 0.0472 mL | 0.2360 mL | 0.4720 mL | 1.1800 mL | |
| 50 mM | 0.0378 mL | 0.1888 mL | 0.3776 mL | 0.9440 mL | |
| 60 mM | 0.0315 mL | 0.1573 mL | 0.3147 mL | 0.7867 mL | |
| 80 mM | 0.0236 mL | 0.1180 mL | 0.2360 mL | 0.5900 mL | |
| 100 mM | 0.0189 mL | 0.0944 mL | 0.1888 mL | 0.4720 mL |
Ezatiostat Related Classifications
HY-13634A Related Classifications
Powered by Bioz